Anthranilic acid based CCK 1 receptor antagonists: preliminary investigation on their second “touch point”

…, L Mennuni, F Makovec, D Hadjipavlou-Litina

Index: Varnavas, Antonio; Lassiani, Lucia; Valenta, Valentina; Mennuni, Laura; Makovec, Francesco; Hadjipavlou-Litina, Dimitra European Journal of Medicinal Chemistry, 2005 ,  vol. 40,  # 6  p. 563 - 581

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Citation Number: 14

Abstract

In this phase of structure–affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50= 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows ...